Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H26O2 |
Molecular Weight | 298.4192 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@@](O)(C#C)[C@@]1(C)CC[C@]3([H])[C@@]4([H])CCC(=O)C=C4CC[C@@]23[H]
InChI
InChIKey=VIKNJXKGJWUCNN-XGXHKTLJSA-N
InChI=1S/C20H26O2/c1-3-20(22)11-9-18-17-6-4-13-12-14(21)5-7-15(13)16(17)8-10-19(18,20)2/h1,12,15-18,22H,4-11H2,2H3/t15-,16+,17+,18-,19-,20-/m0/s1
Molecular Formula | C20H26O2 |
Molecular Weight | 298.4192 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8520623
https://www.medicines.org.uk/emcmobile/PIL.23891.latest.pdf
http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018405s023lbl.pdf
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8520623
https://www.medicines.org.uk/emcmobile/PIL.23891.latest.pdf
http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018405s023lbl.pdf
Norethisterone (INN, BAN), also known as Norethindrone (USAN) (brand names Micronor, AYGESTIN, numerous others) is a synthetic progestational hormone (progestin) with actions similar to those of progesterone but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. AYGESTIN® is not intended, recommended or approved to be used with oncomitant estrogen therapy in postmenopausal women for endometrial protection. Progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge. Allergic reaction could be: Itching or hives, swelling in your face or hands, swelling or tingling in your mouth or throat, chest tightness, trouble breathing.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6319907
Curator's Comment: Known to be CNS penetrant in rat. Human data not available
Norethindrone affects the levels of opioid petides in the rat brain, but it is not clear whether this action is mediated by direct activity within CNS
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL208 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15189034 |
6.8 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | MICRONOR Approved UseIndications Progestin-only oral contraceptives are indicated for the prevention of pregnancy. 2. Efficacy If used perfectly, the first-year failure rate for progestin-only oral contraceptives is 0.5%. However, the typical failure rate is estimated to be closer to 5%, due to late or omitted pills. Table 1 lists the pregnancy rates for users of all major methods of contraception. Table 1: Percentage of Women Experiencing an Unintended Pregnancy During the First Year of Typical Use and the First Year of Perfect Use of Contraception and the Percentage Continuing Use at the End of the First Year. United States. Adapted from Hatcher et al, 1998, Ref. #1 Emergency Contraceptive Pills: Treatment initiated within 72 hours after unprotected intercourse reduces the risk of pregnancy by at least 75%The treatment schedule is one dose within 72 hours after unprotected intercourse, and a second dose 12 hours after the first dose. The Food and Drug Administration has declared the following brands of oral contraceptives to be safe and effective for emergency contraception: Ovral® (1 dose is 2 white pills), Alesse® (1 dose is 5 pink pills), Nordette® or Levlen® (1 dose is 2 light-orange pills), Lo/Ovral® (1 dose is 4 white pills), Triphasil ® or Tri-Levlen® (1 dose is 4 yellow pills) Lactational Amenorrhea Method: LAM is highly effective, temporary method of contraceptionHowever, to maintain effective protection against pregnancy, another method of contraception must be used as soon as menstruation resumes, the frequency or duration of breastfeeds is reduced, bottle feeds are introduced, or the baby reaches six months of age. Source: Trussell J, Contraceptive efficacy. In Hatcher RA, Trussel J, Stewart F, Cates W, Stewart GK, Kowal D, Guest F, Contraceptive Technology: Seventeenth Revised Edition. New York NY: Irvington Publishers, 1998. % of Women Experiencing an Unintended Pregnancy within the First Year of Use % of Women Continuing Use at One Year Among couples attempting to avoid pregnancy, the percentage who continue to use a method for one year Method (1) Typical UseAmong typical couples who initiate use of a method (not necessarily for the first time), the percentage who experience an accidental pregnancy during the first year if they do not stop use for any other reason (2) Perfect UseAmong couples who initiate use of a method (not necessarily for the first time) and who use it perfectly (both consistently and correctly), the percentage who experience an accidental pregnancy during the first year if they do not stop use for any other reason (3) (4) ChanceThe percents becoming pregnant in columns (2) and (3) are based on data from populations where contraception is not used and from women who cease using contraception in order to become pregnant. Among such populations, about 89% become pregnant within one year. This estimate was lowered slightly (to 85%) to represent the percent who would become pregnant within one year among women now relying on reversible methods of contraception if they abandoned contraception altogether 85 85 SpermicidesFoams, creams, gels, vaginal suppositories, and vaginal film 26 6 40 Periodic abstinence 25 63 Calendar 9 Ovulation Method 3 Sympto-Thermal Cervical mucus (ovulation) method supplemented by calendar in the pre-ovulatory and basal body temperature in the post-ovulatory phases 2 Post-Ovulation 1 CapWith spermicidal cream or jelly Parous Women 40 26 42 Nulliparous Women 20 9 56 Sponge Parous Women 40 20 42 Nulliparous Women 20 9 56 Diaphragm 20 6 56 Withdrawal 19 4 CondomWithout spermicides Female (Reality®) 21 5 56 Male 14 3 61 Pill 5 71 Progestin Only 0.5 Combined 0.1 IUD Progesterone T 2.0 1.5 81 Copper T380A 0.8 0.6 78 LNg 20 0.1 0.1 81 Depo-Provera® 0.3 0.3 70 Norplant® and Norplant-2® 0.05 0.05 88 Female Sterilization 0.5 0.5 100 Male Sterilization 0.15 0.10 100 Norethindrone tablets have not been studied for and are not indicated for use in emergency contraception. Launch Date9.4780801E10 |
|||
Primary | AYGESTIN Approved UseAYGESTIN® is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. AYGESTIN® is not intended, recommended or approved to be used with concomitant estrogen therapy in postmenopausal women for endometrial protection. Launch Date3.88108812E11 |
|||
Primary | AYGESTIN Approved UseAYGESTIN® is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. AYGESTIN® is not intended, recommended or approved to be used with concomitant estrogen therapy in postmenopausal women for endometrial protection. Launch Date3.88108812E11 |
|||
Primary | AYGESTIN Approved UseAYGESTIN® is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. AYGESTIN® is not intended, recommended or approved to be used with concomitant estrogen therapy in postmenopausal women for endometrial protection. Launch Date3.88108812E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26.19 ng/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
NORETHINDRONE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
166.9 ng × h/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
NORETHINDRONE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.51 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
NORETHINDRONE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: FEMALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3% |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
NORETHINDRONE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: FEMALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
15 mg 1 times / day multiple, oral Studied dose Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Sources: |
unhealthy, 10.2-41.9 years Health Status: unhealthy Condition: Endometriosis Age Group: 10.2-41.9 years Sex: F Sources: |
Other AEs: Weight gain... |
20 uCi single, intravenous Dose: 20 uCi Route: intravenous Route: single Dose: 20 uCi Sources: |
healthy, 25-35 years n = 6 Health Status: healthy Age Group: 25-35 years Sex: F Population Size: 6 Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Weight gain | 15 mg 1 times / day multiple, oral Studied dose Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Sources: |
unhealthy, 10.2-41.9 years Health Status: unhealthy Condition: Endometriosis Age Group: 10.2-41.9 years Sex: F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 9.0 |
weak [IC50 46 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/15290871/ Page: 1.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 2.0 |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/18356043/ Page: 2.0 |
yes | |||
Sources: https://hmdb.ca/metabolites/HMDB0014855 |
yes | |||
Sources: https://hmdb.ca/metabolites/HMDB0014855 |
yes | |||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Induction of estrogen receptor-alpha and -beta activities by synthetic progestins. | 2000 Apr |
|
[A clinical assessment of a 3 month replacement therapy effectiveness with low norethisterone acetate (Activelle) in postmenopausal women]. | 2001 |
|
[Hormone replacement therapy in women with arterial hypertension in peri- and postmenopause: hemodynamic effects]. | 2001 |
|
Biphasic versus triphasic oral contraceptives for contraception. | 2001 |
|
Biphasic versus monophasic oral contraceptives for contraception. | 2001 |
|
Counting the costs: comparing depot medroxyprogesterone acetate and norethisterone oenanthate utilisation patterns in South Africa. | 2001 |
|
Effects of 17 beta-estradiol and trimegestone alone, and in combination, on the bone and uterus of ovariectomized rats. | 2001 Aug |
|
Preclinical profiles of progestins used in formulations of oral contraceptives and hormone replacement therapy. | 2001 Aug |
|
Evaluation of interaction between fluconazole and an oral contraceptive in healthy women. | 2001 Aug |
|
Pharmacology and toxicology of ethinyl estradiol and norethindrone acetate in experimental animals. | 2001 Aug |
|
Comparison between 1 year oral and transdermal oestradiol and sequential norethisterone acetate on circulating concentrations of leptin in postmenopausal women. | 2001 Aug |
|
Effects of hormone replacement therapy and high-impact physical exercise on skeletal muscle in post-menopausal women: a randomized placebo-controlled study. | 2001 Aug |
|
Heparan sulfate mimetics modulate calpain activity during rat Soleus muscle regeneration. | 2001 Aug |
|
Omental pregnancy in a woman taking the progestogen-only pill. | 2001 Dec |
|
The effect of continuous combined hormone replacement therapy on arterial reactivity in postmenopausal women with established angina pectoris. | 2001 Dec |
|
Sex steroids used in hormonal treatment increase vascular procoagulant activity by inducing thrombin receptor (PAR-1) expression: role of the glucocorticoid receptor. | 2001 Dec 4 |
|
Fine structure of prolactin cell of female albino rat as affected by some antifertility drugs--a comparative electron microscopic study. | 2001 Feb |
|
Effect of trimegestone alone or in combination with estradiol on bone mass and bone turnover in an adult rat model of osteopenia. | 2001 Feb |
|
The insulin-like growth factor-I system and hormone replacement therapy. | 2001 Feb |
|
Effects of oral combined hormone replacement therapy on platelet aggregation in postmenopausal women. | 2001 Feb |
|
Reduced free IGF-I and increased IGFBP-3 proteolysis in Turner syndrome: modulation by female sex steroids. | 2001 Feb |
|
Solution structure and dynamics of an open beta-sheet, glycolytic enzyme, monomeric 23.7 kDa phosphoglycerate mutase from Schizosaccharomyces pombe. | 2001 Feb 16 |
|
[Add back therapy for patients with endometriosis]. | 2001 Jan |
|
Temporal changes in cardiac function and cerebral blood flow during sequential postmenopausal hormone replacement. | 2001 Jan |
|
Charcoal treatment and risk of escape ovulation in oral contraceptive users. | 2001 Jan |
|
Multicenter, comparative study of cycle control, efficacy and tolerability of two low-dose oral contraceptives containing 20 microg ethinylestradiol/100 microg levonorgestrel and 20 microg ethinylestradiol/500 microg norethisterone. | 2001 Jul |
|
Ovarian function during and after treatment with the new progestagen Org 30659. | 2001 Jul |
|
Evaluation of genotoxic potential of synthetic progestins-norethindrone and norgestrel in human lymphocytes in vitro. | 2001 Jul 25 |
|
Continuous combined hormone replacement therapy with oral 17beta-estradiol and norethisterone acetate improves homocysteine metabolism in postmenopausal women. | 2001 Jul-Aug |
|
Comparison of a novel norgestimate/ethinyl estradiol oral contraceptive (Ortho Tri-Cyclen Lo) with the oral contraceptive Loestrin Fe 1/20. | 2001 Jun |
|
Sensitivity to a neurosteroid is increased during addition of progestagen to postmenopausal hormone replacement therapy. | 2001 Jun |
|
Effects of a monthly injectable steroidal contraceptive, Mesigyna, on menstrual pattern, lipoproteins, and coagulation parameters. | 2001 Mar |
|
The effects of transdermal estradiol in combination with oral norethisterone on lipoproteins, coagulation, and endothelial markers in postmenopausal women with type 2 diabetes: a randomized, placebo-controlled study. | 2001 Mar |
|
Determination of steroid sex hormones and related synthetic compounds considered as endocrine disrupters in water by fully automated on-line solid-phase extraction-liquid chromatography-diode array detection. | 2001 Mar 16 |
|
Effects of postmenopausal hormone replacement therapy on lipid, lipoprotein, and apolipoprotein (a) concentrations: analysis of studies published from 1974-2000. | 2001 May |
|
Effects of oral and transdermal hormone replacement therapy on internal carotid artery pulsatility indices in postmenopausal women. A prospective, randomized, comparative study. | 2001 Nov |
|
Monitoring of solid-phase organic synthesis on macroscopic supports by high-resolution magic angle spinning NMR. | 2001 Nov-Dec |
|
Impact of oral contraceptive use on APC-resistance: a prospective, randomized clinical trial with three low-dose preparations. | 2001 Oct |
|
Estimation of hormone replacement therapy influence on serum galanin level in postmenopausal women. | 2001 Sep |
|
Validity of radioimmunological methods for determining free testosterone in serum. | 2001 Sep |
|
Mammographic density changes during different postmenopausal hormone replacement therapies. | 2001 Sep |
|
Influence of postmenopausal hormone replacement therapy on platelet serotonin uptake site and serotonin 2A receptor binding. | 2001 Sep |
|
Progesterone and norethisterone have different effects on tachykinin-like immunoreactivity in rat cortex and striatum. | 2001 Sep 15 |
|
Unscheduled bleeding during initiation of continuous combined hormone replacement therapy: a direct comparison of two combinations of norethindrone acetate and ethinyl estradiol to medroxyprogesterone acetate and conjugated equine estrogens. | 2001 Sep-Oct |
Sample Use Guides
Secondary amenorrhea, abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology: 2.5 to 10 mg may be given daily for 5 to 10 days to produce secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen.
Endometriosis: Initial daily dosage of 5 mg for two weeks. Dosage should be increased by 2.5 mg per day every two weeks until 15 mg per day.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1834933
Curator's Comment: Growth of MCF-7 cells was stimulated by norethindrone (10(-8)-10(-5) M), with maximal growth stimulation at 10(-7) M norethindrone after 7 days of treatment
10 - 10000 nM norethindrone stimulates growth of MCF-7 cells
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 22:41:34 UTC 2023
by
admin
on
Wed Jul 05 22:41:34 UTC 2023
|
Record UNII |
T18F433X4S
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Official Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000175602
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
18.3.1 (ETH/NOR)
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
NCI_THESAURUS |
C776
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
LIVERTOX |
696
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03AA05
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03AC01
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
NDF-RT |
N0000011301
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-ATC |
G03AC01
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03FA01
Created by
admin on Wed Jul 05 22:41:35 UTC 2023 , Edited by admin on Wed Jul 05 22:41:35 UTC 2023
|
||
|
WHO-ATC |
G03FA01
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03AB04
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-ATC |
G03FB05
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03DC02
Created by
admin on Wed Jul 05 22:41:35 UTC 2023 , Edited by admin on Wed Jul 05 22:41:35 UTC 2023
|
||
|
WHO-ATC |
G03DC02
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-VATC |
QG03FB05
Created by
admin on Wed Jul 05 22:41:35 UTC 2023 , Edited by admin on Wed Jul 05 22:41:35 UTC 2023
|
||
|
WHO-ATC |
G03AA05
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
||
|
WHO-ATC |
G03AB04
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
9564
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
SUB09362MIG
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
2880
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
NORETHINDRONE
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | Description: A white or creamy white, crystalline powder; odourless. Solubility: Practically insoluble in water; soluble in 150 parts of ethanol (~750 g/l) TS and in 80 parts of acetone R. Category: Progestational steroid. Storage: Norethisterone should be kept in a well-closed container, protected from light.Definition: Norethisterone contains not less than 97.0% and not more than 103.0% of C20H26O2, calculated with reference to thedried substance. | ||
|
6230
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
T18F433X4S
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
1962
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
1469005
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
3370
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
SUB87911
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
T18F433X4S
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
D009640
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
7514
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | RxNorm | ||
|
100000092090
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
C62059
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
CHEMBL1162
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
M8056
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | Merck Index | ||
|
200-681-6
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
687
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
DTXSID9023380
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
DB00717
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
Norethindrone
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
68-22-4
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY | |||
|
NORETHISTERONE
Created by
admin on Wed Jul 05 22:41:35 UTC 2023 , Edited by admin on Wed Jul 05 22:41:35 UTC 2023
|
PRIMARY | |||
|
7627
Created by
admin on Wed Jul 05 22:41:34 UTC 2023 , Edited by admin on Wed Jul 05 22:41:34 UTC 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE LESS ACTIVE -> PARENT |
Relative Binding Affinity (RBA) to Human Progesterone receptor (cytosol of human breast MCF-7 cells); Unit: % (relative to Org-2058 (=100%)); Norethindrone was 21.5%
IN-VITRO
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 25mg single oral administration (one woman); blood was obtained 3hr after ingestion
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 25mg single oral administration (one woman); blood was obtained 3hr after ingestion
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 3hr after 25mg single oral administration
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL (expressed as a mixture of the 3- (predominant) and 17-sulfate); 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
Unit: ng/ml; 25mg single oral administration (one female); blood was obtained 3hr after the oral ingestion
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
unit: ng/mL; 25mg single oral administration; blood sampled after 3hr
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg/24hr; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
unit: mcg/24h; 1mg q.d. oral administration (w/50mcg estranol); blood sampled on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 25mg single oral administration (one woman); blood was obtained 3hr after ingestion
IN-VIVO
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
Trace amount; Unit: mcg in a urine pool (2.5% aliquot from each of 4days of urine); 25mg q.d. oral administration (one woman)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 2mg (w/0.1mg mestranol) q.d. oral administration; blood was taken 3hr after the tenth pill ingestion on day 14 of the cycle (one woman)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg/24hr; 1mg (w/50mgg mestranol) q.d. oral administration sampled on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg/24hr; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
<2 to 12; Unit: ng/mL; 1mg (50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg/24hr; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (w/50mcg mestranol) q.d. oral administration sampled on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
<2; Unit: mcg/24hr; 1mg (50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg in pooled urine (2.5% aliquot from each of the 4 days urine); 25mg q.d. oral administration for 4 days (one woman)
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (w/50mcg mestranol) q.d. oral administration sampled on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
||
|
PARENT -> METABOLITE |
Metabolite to parent drug ratio in non-uraemic human plasma.
Norethynodrel is metabolized in man to the antifertility agent norethisterone(norethindrone).
METABOLITE TO PARENT DRUG RATIO
PLASMA; URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/ml; 2mg (w/0.1mg mestranol) q.d. oral administration (one woman); blood was taken 3hr after ingestion of the tenth pill on day 14 of the cycle
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: mcg in a urine pool (2.5% aliquot from each of 4 days of urine); 25mg q.d. oral administration for 4 days
IN-VIVO
URINE
|
||
|
METABOLITE LESS ACTIVE -> PARENT |
Unit: ng/mL; 2mg (w/0.1mg mestranol) q.d. oral administration; blood was obtained 3hr after the tenth pill administration on day 14 of the cycle
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
Unit: ng/mL; 1mg (w/50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
PLASMA
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
IN-VIVO
URINE
|
||
|
METABOLITE INACTIVE -> PARENT |
<2; Unit: mcg/24hr; 1mg (50mcg mestranol) q.d. oral administration; analyzed on the 7th, 14th, and 21st days (two females)
IN-VIVO
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
|
Elimination PHARMACOKINETIC |
|
||
Volume of Distribution | PHARMACOKINETIC |
|
|
|||